Wednesday 25 January 2006
ConjuChem's PC-DAC(TM):Exendin-4 Advancing into Human Clinical Testing For Type 2 Diabetes
- FDA Submission filed, Clinical Program to Start in March 2006 -
MONTREAL, Jan. 25 - ConjuChem Inc. (TSX: CJC) today announced it
has filed with the U.S. Food and Drug Administration (FDA) a submission to
initiate a Phase I/II trial for the treatment of Type 2 diabetes using the
Company's proprietary PC-DAC(TM):Exendin-4 compound. Regulatory clearance is
anticipated prior to the end of February 2006 with patient enrollment starting
in March 2006. Preliminary data is expected to be available at the end of the
second quarter of calendar 2006.
Phase I/II Trial Design
The Phase I/II trial will be a randomized, double-blind, single
escalating dose study that will evaluate the safety, tolerability, maximum
tolerated dose (MTD), pharmacokinetic and pharmacodynamic (duration of
activity after one injection) profile of PC-DAC(TM):Exendin-4 in patients with
stable Type 2 diabetes with HbA1c levels between 6.5% - 11%. Enrolling a
maximum of 68 patients, the study will consist of six cohorts (plus two
optional cohorts) and a MTD cohort.
"We anticipate this study with PC-DAC(TM):Exendin-4 will confirm the
positive efficacy and the excellent tolerability profile we saw for this
compound in pre-clinical studies," said Dr. Jean-Paul Castaigne, Chief
Operating Officer. "Moreover, we expect the data to support our efforts to
produce a once-per-week GLP-1 receptor agonist compound."
Following the completion of this study, ConjuChem intends to start a
phase I/II multiple dose trial.
About PC-DAC(TM):Exendin-4
Exendin-4 is a Glucagon-like peptide-1 (GLP-1) homolog and an agonist for
the GLP-1 receptor. It lowers the blood glucose levels through a distinct
mechanism complementary to the mechanisms of action of currently available
anti-diabetic drugs. By decreasing glucagon and increasing insulin secretion
in a glucose-dependent manner, Exendin-4 may stimulate (B)-cell proliferation,
restore (B)-cell sensitivity to glucose, delay gastric emptying, and increase
peripheral sensitivity to glucose. Historically, the clinical utility of
Exendin-4 was limited by its relatively short half-life in plasma. Developed
with ConjuChem's proprietary technology, PC-DAC(TM):Exendin-4 is a modified
Exendin-4 analogue that is bonded to recombinant human albumin. This preformed
conjugate has a much longer half-life (up to one week) than its natural
counterpart. In addition, by conjugating exendin-4 to albumin ex-vivo (PC-
DAC:Exendin-4), ConjuChem expects to control the pharmacokinetic surge of drug
responsible for causing nausea and vomiting in patients and, to shield the
exendin-4 peptide from immune system recognition.
About PC-DAC(TM)
ConjuChem developed Preformed Conjugate-Drug Affinity Complex (PC-
DAC(TM)) to complement its Drug Affinity Complex (DAC(TM)) technology.
Preformed conjugates are a natural extension of the Company's core albumin
bonding expertise. Both DAC(TM) and PC-DAC(TM) peptides are designed to have
much longer durations of activity while retaining the therapeutic properties
of the original peptides.
PC-DAC(TM):Peptides are engineered such that the DAC(TM):Peptide attaches
covalently to recombinant human albumin outside the body (ex vivo
bioconjugation). The PC-DAC(TM):Peptide is subsequently injected
subcutaneously into a patient. Ex vivo bioconjugation of preformed conjugates
only recently became a viable option with the introduction of a recombinant
source of albumin. Previously, the only available albumin was purified from
human serum, which could not be used as part of a drug product due to safety
concerns inherent to the source.
About ConjuChem
ConjuChem, developers of next generation medicines from therapeutic
peptides, is creating long-acting compounds based on bioconjugation platform
technologies. When applied to peptides, the Company's systemic DAC(TM)
Technologies enable the creation of new drugs with significantly enhanced
therapeutic properties as compared to the original peptide. The Company is
developing compounds to treat various disorders including diabetes, human
growth deficiencies, HIV/AIDS, and congestive heart failure.
Detailed descriptions of the Company can be viewed on the Company's
website www.conjuchem.com.